Literature DB >> 28917148

Self-nanoemulsifying drug delivery systems of myricetin: Formulation development, characterization, and in vitro and in vivo evaluation.

Jin Qian1, Houjun Meng2, Lei Xin1, Mengxin Xia1, Hongyi Shen1, Guowen Li3, Yan Xie4.   

Abstract

Despite various pharmacological effects, myricetin (Myr) shows low oral bioavailability (<10%) due to its poor solubility, which limits its applications. To address this problem, self-nanoemulsifying drug delivery systems (SNEDDS) were developed by investigating the solubility of Myr in various excipients, constructing pseudo-ternary phase diagrams, and optimizing based on droplet size and emulsification efficacy after drug loading. The obtained Myr-SNEDDS were F04 (Capryol 90/Cremophor RH 40/PEG 400 4:3:3), F08 (Capryol 90/CremophorRH40/1,2-propanediol 4:3:3), F13 (Capryol 90/Cremophor EL/Transcutol HP 4:3:3) and F15 (Capryol 90/Cremephor RH 40/Transcutol HP 2:7:1), with droplet sizes less than 200nm. Additional evaluations showed that these Myr-SNEDDS formulations had fast release properties (over 90% in 1min), low cytotoxicity, and improved permeability and solubility compared with the free drug. Consequently, the oral bioavailabilities of Myr were 5.13, 6.33, 4.69 and 2.53-fold for F04, F08, F13 and F15, respectively, relative to Myr alone. The present study demonstrated that SNEDDS is a viable platform for the oral delivery of insoluble drugs such as Myr.
Copyright © 2017 Elsevier B.V. All rights reserved.

Entities:  

Keywords:  Intestinal permeability; Myricetin; Oral bioavailability; Poor solubility; SNEDDS

Mesh:

Substances:

Year:  2017        PMID: 28917148     DOI: 10.1016/j.colsurfb.2017.09.020

Source DB:  PubMed          Journal:  Colloids Surf B Biointerfaces        ISSN: 0927-7765            Impact factor:   5.268


  14 in total

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